ActiTarg Series · over 6,600 compounds
ActiTarg-K Kinase Modulators
A screening set of molecules that contain chemical lattices present in compounds reported to possess protein kinase inhibiting properties. There are over 6,600 compounds in this collection.
ActiTarg-K6600 represents a variety of chemical series. Structural constraints and novel pendants provide variability for hit optimization. A top diversity selection of 960 compounds, ActiTarg-K960, is a pre-filtered 12-plate set for smaller kinase screens. Compounds are available for cherry-picking and/or as a collection in 96- or 384-well plates and in vials.
Among strategies in cancer therapeutics, protein kinase inhibition is a viable approach, stimulated by the role this family of phosphorylating enzymes plays in proliferative processes and by agents such as imatinib (Gleevec) in chronic myeloid leukemia and certain solid tumors. Along with that tyrosine kinase inhibitor, other agents that inhibit this and other cell-cycle-regulating kinases (CDKs) have been developed for cancer and immune-system disorders.
Lattices represented
| Kinase context | Lattice type |
|---|---|
| Tyrosine / CDK | Various |
| CDK | Adenines; flavones; isoflavones; 2-aminothiazoles |
| p38 MAP | 4,5-Diarylimidazoles |
| Raf | Diarylureas |
| Ser/Thr | NaphthSONH |
| PASS* >0.50 subsets | CDK isoxazolidinine and aminothiazole; tyrosine; p38MAP; PKC |
*PASS: software that predicts biological activity based on structural similarity to compounds reported to have the specified activity.
Published screens that used ActiTarg-K
These are literature reports, not TimTec efficacy claims:
- Serra-Roma, A.; Shakhova, O. Identification of novel small-molecule kinase modulators for the treatment of neuroblastoma. Oncol. Ther. 2020. doi:10.1007/s40487-020-00113-5. HTS of ActiTarg-K960 (TimTec Inc.), the 960-compound diversity subset of ActiTarg-K.
ActiTarg is one of TimTec’s targeted series. See the ActiTarg Series for the other letter collections.